ML329 is a micropthalmia-associated transcription factor (MITF) inhibitor, which inhibits TRPM-1 promoter activity with an IC50 of 1.2 μM.
ML329 inhibits the expression of numerous micropthalmia-associated transcription factor (MITF) target genes and blocks the proliferation of numerous cell lines that require MITF for proliferation. ML329 could directly or indirectly interact with MITF or components of the MITF regulatory network. As a transcription factor that regulates cell cycle and pigmentation, interference of MITF with ML329 will be useful in characterizing the specific roles of MITF in melanoma and validate blockade of MITF function as a potential treatment of melanoma. ML329 shows specific activity against the MITF-dependent cells, primary melanocytes but no effect on the viability in A375 cells. ML329 reduces the expression of multiple MITF target genes, including pigment-related genes and the cell cycle regulator CDK2. As a tool compound, ML329 will be useful in elucidating the role of MITF in melanocyte lineage development and in melanoma disease progression[1].
References:
[1]. Faloon PW, et al. A Small Molecule Inhibitor of the MITF Molecular Pathway. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2012 Dec 13.